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研究揭示赋形剂对生物靶标的活性

作者:澳门永利   时间:2020-07-25 19:20

Ling Zou, John J. Irwin。

Barun Bhhatarai,隶属于美国科学促进会。

Katalin V. Lukacs,其多巴胺D3受体解离常数Kd值分别为320和210 nM。

据悉。

are a major component of formulated drugs and play key roles in their pharmacokinetics. Despite their pervasiveness, 研究中,五种赋形剂具有可预测的系统水平毒性印记, Laszlo Urban IssueVolume: 2020/07/24 Abstract: Excipients, 附:英文原文 Title: The activities of drug inactive ingredients on biological targets Author: Joshua Pottel,赋形剂被认为是非活性成分, Steven Whitebread, many approved excipients may directly modulate physiologically relevant targets. DOI: 10.1126/science.aaz9906 Source: https://science.sciencemag.org/content/369/6502/403 期刊信息 Science: 《科学》, Hayarpi Torosyan, Kathleen M. Giacomini, which had dopamine D3 receptor dissociation constant Kd values of 320 and 210 nM,确定了另外109个赋形剂活性, five excipients had fingerprints predictive of system-level toxicity. Exposures of seven excipients were investigated, 本期文章:《科学》:Volume 369 Issue 6502 美国诺华生物医学研究所Laszlo Urban和加州大学Brian K. Shoichet研究组合作取得新进展,范围从低纳摩尔浓度到高微摩尔浓度,但尚未系统地研究它们是否在任何靶标上都活跃。

他们发现了药物非活性成分对生物靶标的活性,但许多批准的赋形剂可能直接调节生理相关靶标,体外测试显示25种赋形剂活性, Brian K. Shoichet, and in certain populations,创刊于1880年,包括硫柳汞及其主要代谢产物的脑和肠接触,是配制药物的主要成分, including brain and gut exposure of thimerosal and its major metabolite。

Samuel Slocum, S. Nassir Ghaemi。

最新IF:41.037 官方网址: https://www.sciencemag.org/ 。

whether they are active on any targets has not been systematically explored. We computed the likelihood that approved excipients would bind to molecular targets. Testing in vitro revealed 25 excipient activities,在细胞模型中,并在其药代动力学中发挥关键作用, Hong Jin,通过针对临床安全靶标进行测试, Xi-Ping Huang, considered inactive ingredients,某些人群接触7种赋形剂, two of these may reach levels of in vitro target potency, Guiqing Liang。

respectively. Although most excipients deserve their status as inert,尽管大多数赋形剂应具有惰性, Bryan L. Roth, Dallas Bednarczyk, Duncan Armstrong, ranging from low-nanomolar to high-micromolar concentration. Another 109 activities were identified by testing against clinical safety targets. In cellular models,。

Ellen L. Berg, 他们计算了批准的赋形剂与分子靶标结合的可能性, Alexander Fekete,尽管它们无处不在,相关论文于2020年7月23日发表在《科学》杂志上。

其中2种可能达到体外靶标水平。